http://www.cnr.it/ontology/cnr/individuo/prodotto/ID19337
N-palmitoyl-vanillamide (palvanil) is a non-pungent analogue of capsaicin with stronger desensitizing capability against the TRPV1 receptor and potential anti-hyperalgesic activity (Articolo in rivista)
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- N-palmitoyl-vanillamide (palvanil) is a non-pungent analogue of capsaicin with stronger desensitizing capability against the TRPV1 receptor and potential anti-hyperalgesic activity (Articolo in rivista) (literal)
- Anno
- 2011-01-01T00:00:00+01:00 (literal)
- Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
- 10.1016/j.phrs.2010.12.019 (literal)
- Alternative label
De Petrocellis L., Guida F., Schiano Moriello A., De Chiaro M., Piscitelli F., de Novellis V., Maione S., and Di Marzo V. (2011)
N-palmitoyl-vanillamide (palvanil) is a non-pungent analogue of capsaicin with stronger desensitizing capability against the TRPV1 receptor and potential anti-hyperalgesic activity
in Pharmacological research (Print)
(literal)
- Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
- De Petrocellis L., Guida F., Schiano Moriello A., De Chiaro M., Piscitelli F., de Novellis V., Maione S., and Di Marzo V. (literal)
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- Pagina fine
- Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume
- Rivista
- Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#note
- Pharmacological Research 63 (2011) 294-299. (literal)
- Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroFascicolo
- Note
- ISI Web of Science (WOS) (literal)
- Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
- Titolo
- N-palmitoyl-vanillamide (palvanil) is a non-pungent analogue of capsaicin with stronger desensitizing capability against the TRPV1 receptor and potential anti-hyperalgesic activity (literal)
- Abstract
- N-acyl-vanillamide (NAVAM) analogues of the natural pungent principle of
capsicum, capsaicin, were developed several years ago as potential non-pungent analgesic
compounds. N-oleoyl-vanillamide (olvanil) and N-arachidonoy-vanillamide (arvanil), in
particular, were described in several publications and patents to behave as potent
anti-hyperalgesic compounds in experimental models of chronic and inflammatory pain, and
to activate both \"capsaicin receptors\", i.e. the transient receptor potential of
vanilloid type-1 (TRPV1) channel, and, either directly or indirectly, cannabinoid
receptors of type-1. Here we report the biochemical and pharmacological characterization
of a so far neglected NAVAM, N-palmitoyl-vanillamide (palvanil), and propose its possible
use instead of capsaicin, as a possible topical analgesic. Palvanil exhibited a kinetics
of activation of human recombinant TRPV1-mediated intracellular calcium elevation
significantly slower than that of capsaicin (t(1/2) = 21 s and 8 s, respectively at 1 mu
M). Slow kinetics of TRPV1 agonists were previously found to be associated with stronger
potencies as TRPV1 desensitizing agents, which in turn are usually associated with lower
pungency and stronger anti-hyperalgesic activity. Accordingly, palvanil desensitized the
human recombinant TRPV1 to the effect of capsaicin (10 nM) with significantly higher
potency than capsaicin (IC(50) = 0.8 nM and 3.8 nM, respectively), this effect reaching
its maximum more rapidly (50 and 250 min, respectively). Palvanil was also more potent
than capsaicin at desensitizing the stimulatory effect of TRPV1 by low pH together with
anandamide, which mimics conditions occurring during inflammation. In the eye-wiping
assay carried out in mice, palvanil was not pungent and instead caused a strong and
long-lasting inhibition of capsaicin-induced eye-wiping. Finally, intraplantar palvanil
inhibited the second phase of the nociceptive response to formalin in mice. In
conclusion, palvanil appears to be a non-pungent analogue of capsaicin with stronger
desensitizing effects on TRPV1 and hence potentially higher anti-hyperalgesic activity. (literal)
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